| Isifundo se-in vitro | I-Bosutinib inokukhetha okuphezulu kwe-Src kune-non-Src family kinases, ene-IC50 ye-1.2 nM, futhi ivimbela ngempumelelo ukwanda kwamaseli ancike ku-Src, nge-IC50 ye-100 nM. I-Bosutinib ivimbele ngokuphawulekayo ukwanda kwemigqa yeseli leukemia ye-Bcr-Abl-positive KU812, K562, ne-MEG-01 kodwa hhayi i-Molt-4, HL-60, Ramos, kanye nezinye imigqa yeseli ye-leukemia, ne-IC50 ye-5 nM, 20 nM, ngokulandelanayo. , kanye no-20 nM, kusebenza kangcono kune-STI-571. Ngokufanayo ne-STI-571, i-Bosutinib isebenza kumafayibha aguqulayo e-Abl-MLV futhi inomsebenzi okhulayo nge-IC50 ye-90 nM. Ekugxiliseni okungu-50 nM, 10-25 nM, kanye no-200 nM, ngokulandelana, i-Bosutinib ikhiphe i-Bcr-Abl ne-STAT5 kumaseli e-CML kanye ne-v-Abl tyrosine phosphorylation evezwa kumafayibha, lokhu kuphumela ekuvinjweni kwe-phosphorylation ye-Bcr-Abl esiginali yezansi nomfula. /Hk. Nakuba ingakwazi ukuvimbela ukwanda nokusinda kwamangqamuzana omdlavuza webele, inganciphisa kakhulu ukunyakaza nokuhlasela kwamangqamuzana omdlavuza webele, i-IC50 i-250 nM, futhi ithuthukise ukunamathela kwe-intercellular kanye ne-membrane yendawo ye-β-catenin. |
| Isifundo se-vivo | I-Bosutinib yayisebenza kahle kumagundane anqunu aphethe i-Src-transformed fiber xenografts kanye ne-HT29 xenografts ngedosi engu-60 mg/kg ngosuku, ngamavelu e-T/C angu-18% no-30%, ngokulandelana. Ukuphathwa ngomlomo kwe-Bosutinib kumagundane izinsuku ezi-5 kuvimbe kakhulu ukukhula kwamathumba e-K562 ngendlela encike kumthamo. Izimila ezinkulu zaqedwa ngomthamo we-100 mg / kg, ukwelashwa ngesilinganiso se-150 mg / kg kukhishwe izimila ezingenabo ubuthi. Uma kuqhathaniswa nomthelela ku-HT29 isimila esifakwe kabusha, i-Bosutinib ngethamo lika-75 mg/kg, kabili ngosuku, ingavimbela ukukhula kwesimila kumagundane anqunu athwele isimila esifakwe i-Colo205, awubanga khona umphumela ophakeme ngemva kokwenyusa umthamo, kodwa i-50 mg/ kg umthamo awubanga namphumela. |
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